Tapentadol (i.e., 3-[(1R,2R)-3-(dimethyamino)-1-ethyl-2-methylpropyl]phenol) is a small organic molecule that is used as an analgesic. Tapentadol is known to have a dual mechanism of action as an agonist of the μ-opioid receptor and also as a norepinephrine (NE) reuptake inhibitor (NRI) for improved analgesic efficacy especially in chronic or neuropathic pain disorders.
Several different routes for preparing tapentadol have been reported. A typical method is to produce a racemic mixture of intermediates that must be separated by chiral chromatographic separation or by chiral resolution. The separation of chiral compounds, however, can be technically challenging, time consuming, or both. What is needed, therefore, is a process for preparing tapentadol that does not require chiral separation or chiral resolution, but rather relies on a direct asymmetric synthesis of chiral compounds. Such an enantioselective synthesis process would facilitate the production of tapentadol by reducing costs and saving time.